A Review of the Receptor Binding and Pharmacological Effects of <i>N</i>‐methyltyramine

Stohs, Sidney J.; Hartman, Michael J.

doi:10.1002/ptr.5231

Cited by 23 publications

(14 citation statements)

References 20 publications

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“…In conclusion, our observations in WAT, heart, muscles and plasma indicated that phenelzine did not increase the risk of lipotoxicity or cardiovascular disease in mice. The lack of increased lipid mobilization after phenelzine treatment agrees with an expected increase of tyramine content because this compound lacks strong lipolytic effect, in contrast to its derivative N‐methyltyramine (Stohs and Hartman, ). Thus, one can expect that phenelzine is not solely blocking MAO in nervous and cardiovascular systems, as it is capable of modulating carbohydrate and lipid metabolism in other tissues by interfering at least with H 2 O 2 metabolism, SSAO and PEPCK activities.…”

Section: Discussionsupporting

confidence: 73%

Body fat reduction without cardiovascular changes in mice after oral treatment with the MAO inhibitor phenelzine

Carpéné

Mercader

Gonidec

et al. 2018

British J Pharmacology

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Section: Discussionsupporting

confidence: 73%

Body fat reduction without cardiovascular changes in mice after oral treatment with the MAO inhibitor phenelzine

Carpéné

Mercader

Gonidec

et al. 2018

British J Pharmacology

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“…() also showed that, in human and rat adipocytes tyramine and N ‐methyltyramine, minor components found in bitter orange extract inhibited lipolysis in contrast to p‐ synephrine. A review of the adrenergic receptor binding and effects of N ‐methyltyramine indicate that it acts as an α‐adrenergic receptor antagonist while promoting appetite and inhibiting lipolysis, effects counter to commonly perceived ideas regarding its use in dietary supplements (Stohs and Hartman, ).…”

Section: Mechanistic Studiesmentioning

confidence: 83%

Safety, Efficacy, and Mechanistic Studies Regarding Citrus aurantium (Bitter Orange) Extract and p‐Synephrine

Stohs

2017

Phytotherapy Research

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Citrus aurantium L. (bitter orange) extracts that contain p‐synephrine as the primary protoalkaloid are widely used for weight loss/weight management, sports performance, appetite control, energy, and mental focus and cognition. Questions have been raised about the safety of p‐synephrine because it has some structural similarity to ephedrine. This review focuses on current human, animal, in vitro, and mechanistic studies that address the safety, efficacy, and mechanisms of action of bitter orange extracts and p‐synephrine. Numerous studies have been conducted with respect to p‐synephrine and bitter orange extract because ephedra and ephedrine were banned from use in dietary supplements in 2004. Approximately 30 human studies indicate that p‐synephrine and bitter orange extracts do not result in cardiovascular effects and do not act as stimulants at commonly used doses. Mechanistic studies suggest that p‐synephrine exerts its effects through multiple actions, which are discussed. Because p‐synephrine exhibits greater adrenergic receptor binding in rodents than humans, data from animals cannot be directly extrapolated to humans. This review, as well as several other assessments published in recent years, has concluded that bitter orange extract and p‐synephrine are safe for use in dietary supplements and foods at the commonly used doses. Copyright © 2017 The Authors Phytotherapy Research Published by John Wiley & Sons Ltd.

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“…Hordenine stimulates norepinephrine, a hormone that mediates lipid release and can lead to body weight loss and inhibited gut movements, which contributes to decreased weight gain [33,34]. N -methyltyramine is a protoalkaloid isolated from various plant species, and it is assumed to be an adrenergic agonist with pharmacological properties similar to other structurally related biogenic amines, such as p -synephrine, p -octopamine, epinephrine, and norepinephrine, as well as ephedrine and amphetamine, which are phenylpropylamine derivatives [35]. Moreover, p -synephrine has been shown to reduce body weight in pre-clinical and clinical studies [33,36].…”

Section: Discussionmentioning

confidence: 99%

Genotoxicity and pharmacokinetic characterization of Cereus jamacaru ethanolic extract in rats

Medeiros

Bortolin

et al. 2019

Bioscience Reports

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The effect of Cereus jamacaru ethanolic extract in rats was analyzed using genotoxicity assays and liver ABCB1 and CYP2D4 gene expression. The lyophilized extract of C. jamacaru cladodes was analyzed with LC–MS/MS. Male Wistar rats (n=36) were equally distributed into six groups that did (+) or did not (−) receive cyclophosphamide treatments: Control (−); Control (+); EXP 1 (−), and EXP 1 (+), both treated with 210 mg/kg of ethanolic extract; and EXP 2 (−) and EXP 2 (+), both treated with 420 mg/kg of ethanolic extract. After 30 d of treatment, body weight and food and water intake were monitored. Right femur of the rats and spinal canal fluid were harvested and used for genotoxicity assays, and the liver samples were used for gene expression studies. The phytochemical analysis identified novel compounds. Animals treated with C. jamacaru showed lower body weight and food ingestion compared to controls (P<0.05). The genotoxicity assay showed an absence of ethanolic extract cytotoxicity. CYP2D4 expression was higher in EXP 2 groups compared with EXP 1 (−) group (P<0.05). ABCB1A expression was higher in negative groups compared with the positive groups. These results indicated a new phytochemical characterization of C. jamacaru and its effect on food ingestion and body weight gain. Moreover, the genotoxicity assay suggested that C. jamacaru ethanolic extract treatment presents significant intrinsic genotoxic potential and the enhanced expression of ABCB1 and CYP2D4 on C. jamacaru extract treatment suggests a role of the efflux transporter and microsomal enzyme, respectively, in C. jamacaru pharmacokinetics.

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A Review of the Receptor Binding and Pharmacological Effects of N‐methyltyramine

Cited by 23 publications

References 20 publications

Body fat reduction without cardiovascular changes in mice after oral treatment with the MAO inhibitor phenelzine

Body fat reduction without cardiovascular changes in mice after oral treatment with the MAO inhibitor phenelzine

Safety, Efficacy, and Mechanistic Studies Regarding Citrus aurantium (Bitter Orange) Extract and p‐Synephrine

Genotoxicity and pharmacokinetic characterization of Cereus jamacaru ethanolic extract in rats

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